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Bupropion
Basic Information
Summary
A frequently prescribed atypical antidepressant. Occasionally prescribed as an aid to smoking cessation. May lower seizure threshold in predisposed individuals. Poorly understood mechanism of action, probably an NDRI. Avoid combination with other drugs.
Stimulant
Stimulants excite the nervous system and increase physiological function.
Read more on TripSit Wiki...Habit-forming
These drugs pose a higher risk of causing habit forming behaviour, take particular care with the amount and frequency they are taken.
Read more on TripSit Wiki...Duration
| Parent | |
|---|---|
| Onset | 15-90 minutes |
| Duration | 11-21 hours |
| After-effects | 1-6 hours |
| Metabolites | |
|---|---|
| Onset | 15-90 minutes |
| Duration | 20-37 hours |
| After-effects | 1-6 hours |
General-effects
Mild - moderate increase in motor activity and agitation/excitement
Adverse-effects
Agitation, dry mouth, insomnia, headache/migraine, nausea/vomiting, constipation, tremor, dizziness, excessive sweating, blurred vision, tachycardia, confusion, rash, hostility, cardiac arrhythmia, and auditory disturbance
Overdose-symptoms
Seizure, hallucinations, loss of consciousness, sinus tachycardia, ECG changes, bradycardia, cardiac failure, cardiac arrest, and death
Warning
Bupropion lowers the seizure threshold and can induce seizures when excessive doses are used and/or when combined with CNS stimulants or other drugs that also lower the threshold, such as theophylline, steroids, some tricyclic antidepressants, and alcohol
Chemistry
IUPAC: (±)-2-(tert-Butylamino)-1-(3-chlorophenyl)propan-1-one | Formula: C13H18ClNO | Molecular Mass: 239.74 g/mol
Pharmacology
NDRI (Norepinephrine-Dopamine Reuptake Inhibitor); NDRA (Norepinephrine-Dopamine Releasing Agent); α3β2, α3β4, α4β2, and α7 nACh receptor antagonist
Pharmacokinetics
Protein Binding: 84% (bupropion), 77% [hydroxybupropion (active metabolite)], 42% [threohydrobupropion (active metabolite)] | Metabolism: hepatic, primarily CYP2B6-mediated hydroxylation; both bupropion and hydroxybupropion (active metabolite) are CYP2D6 inhibitors | Excretion: renal (87%; 0.5% unchanged) and faecal (10%)
Legal
Australia: Prescription Only (S4) | Canada: ℞-only | United Kingdom: POM | United States: ℞-only
Aliases
wellbutrin
zyban
amfebutamone
Contradictions
Seizure disorder, current or prior diagnosis of bulimia or anorexia nervosa, abrupt discontinuation of alcohol, benzodiazepines, barbiturates, and anti-epileptic drugs, and MAOIs,
Interactions
Dangerous
Caution
- Mushrooms
- Stimulants increase anxiety levels and the risk of thought loops which can lead to negative experiences
- LSD
- Stimulants increase anxiety levels and the risk of thought loops which can lead to negative experiences
- DMT
- Stimulants increase anxiety levels and the risk of thought loops which can lead to negative experiences
- Mescaline
- The focus and anxiety caused by stimulants is magnified by psychedelics and results in an increased risk of thought loops
- 2C-x
- The anxiogenic and focusing effects of stimulants increase the chance of unpleasant thought loops. The combination is generally uneccessary because of the stimulating effects of psychedelics. Combination of the stimulating effects may be uncomfortable.
- Cannabis
- Stimulants increase anxiety levels and the risk of thought loops which can lead to negative experiences
- Ketamine
- No unexpected interactions, though likely to increase blood pressure but not an issue with sensible doses. Moving around on high doses of this combination may be ill advised due to risk of physical injury.
- MXE
- Risk of tachycardia, hypertension, and manic states
- Cocaine
- This combination of stimulants will increase strain on the heart. It is not generally worth it as cocaine has a mild blocking effect on dopamine releasers like amphetamine
- Caffeine
- This combination of stimulants is not generally necessary and may increase strain on the heart, as well as potentially causing anxiety and greater physical discomfort.
- Alcohol
- Drinking on stimulants is risky because the sedative effects of the alcohol are reduced, and these are what the body uses to gauge drunkenness. This typically leads to excessive drinking with greatly reduced inhibitions, high risk of liver damage and increased dehydration. They will also allow you to drink past a point where you might normally pass out, increasing the risk. If you do decide to do this then you should set a limit of how much you will drink each hour and stick to it, bearing in mind that you will feel the alcohol and the stimulant less. Extended release formulations may severely impede sleep, further worsening the hangover.
- GHB/GBL
- Stimulants increase respiration rate allowing a higher dose of sedatives. If the stimulant wears off first then the opiate may overcome the patient and cause respiratory arrest.
- Opioids
- Stimulants increase respiration rate allowing a higher dose of opiates. If the stimulant wears off first then the opiate may overcome the patient and cause respiratory arrest.
Unsafe
- DOx
- The combined stimulating effects of the two can lead to an uncomfortable body-load, while the focusing effects of amphetamine can easily lead to thought loops. Coming down from amphetamines while the DOx is still active can be quite anxiogenic.
- NBOMes
- Amphetamines and NBOMes both provide considerable stimulation. When combined they can result in tachycardia, hypertension, vasoconstriction and in extreme cases heart failure. The anxiogenic and focusing effects of stimulants are also not good in combination with psychedelics as they can lead to unpleasant thought loops. NBOMes are known to cause seizures and stimulants can increase this risk.
- 2C-T-x
- Stimulants increase anxiety levels and the risk of thought loops which can lead to negative experiences. In extreme cases, they can result in severe vasoconstriction, tachycardia, hypertension, and in extreme cases heart failure.
- 5-MeO-xxT
- The anxiogenic and focusing effects of stimulants increase the chance of unpleasant thought loops. The combination is generally unnecessary because of the stimulating effects of psychedelics.
- DXM
- Both substances raise heart rate, in extreme cases, panic attacks caused by these drugs have led to more serious heart issues.
- PCP
- This combination can easily lead to hypermanic states
Low Risk & No Increased Effects
Low Risk & Decreased Effects
- Benzodiazepines
- Both can dull each other's effects, so if one wears off before the other it's possible to overdose due to the lack of counteraction